| Description | 8-Deoxygartanin is a butyrylcholinesterase (BChE) selective inhibitor, it exhibits significant inhibition of self-induced α2-amyloid (Aα2) aggregation, it has multifunctional activities against Alzheimer's disease (AD) and could be promising compounds for the therapy of AD. |
| In vitro | 本研究采用Ellman's比色法，调查了G. mangostana提取物及其化学成分对乙酰胆碱酯酶（AChE）和丁酰胆碱酯酶（BChE）的抑制活性。通过胆碱酯酶抑制导向方法，成功鉴定出六种具有中等到强大胆碱酯酶抑制活性的前列腺素类黄酮，其IC50值低于20.5 μM。其中，对AChE的高效抑制剂是garcinone C，对BChE的高效抑制剂是γ-mangostin，IC50值分别为1.24μM和1.78μM。在这些黄酮中，mangostanol、3-isomangostin、garcinone C和α±-mangostin为AChE选择性抑制剂，8-Deoxygartanin为BChE选择性抑制剂，而γ-mangostin是双重抑制剂。初步的结构-活性关系研究表明，C-8前列腺素和C-7羟基对于良好的AChE和BChE抑制活性至关重要。酶动力学研究指出，α±-mangostin和garcinone C是混合型抑制剂，而γ-mangostin是AChE的非竞争性抑制剂。相反，γ-mangostin和garcinone C是BChE的非竞争性抑制剂，而α±-mangostin是BChE的混合型抑制剂。 |
| Target activity | p65:11.3 μM (IC50) |
| Synonyms | 8-脱氧藤黄苷 |
| molecular weight | 380.43 |
| Molecular formula | C23H24O5 |
| CAS | 33390-41-9 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 55 mg/mL (144.57 mM) |
| References | 1. Prenylated xanthones from mangosteen as promising cholinesterase inhibitors and their molecular docking studies.Phytomedicine. 2014 Sep 25;21(11):1303-9. |